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ZA888996B - New 11-arylsteroid compounds - Google Patents

New 11-arylsteroid compounds

Info

Publication number
ZA888996B
ZA888996B ZA888996A ZA888996A ZA888996B ZA 888996 B ZA888996 B ZA 888996B ZA 888996 A ZA888996 A ZA 888996A ZA 888996 A ZA888996 A ZA 888996A ZA 888996 B ZA888996 B ZA 888996B
Authority
ZA
South Africa
Prior art keywords
group
hydroxyl
acyloxy
compounds
alkoxy
Prior art date
Application number
ZA888996A
Inventor
Hendrik Paul De Jongh
Paul De Jongh Hendrik
Nicolaas Pieter Van Vliet
Pieter Van Vliet Nicolaas
Original Assignee
Akzo Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Akzo Nv filed Critical Akzo Nv
Publication of ZA888996B publication Critical patent/ZA888996B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Gyroscopes (AREA)
  • Fats And Perfumes (AREA)

Abstract

The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: <CHEM> in which R1 is an aryl group with a - @@@X group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-6 C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom; R2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group; R3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R2 and R3 together form a ring system, with the proviso that if R3 is hydroxyl, R2 is not hydrogen or hydroxyl; and R4 is a methyl or ethyl group; and the alpha - and beta -bonds are indicated by dashed (---) and wedged ( @) lines respectively.
ZA888996A 1987-12-12 1988-11-30 New 11-arylsteroid compounds ZA888996B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
NL8703008 1987-12-12

Publications (1)

Publication Number Publication Date
ZA888996B true ZA888996B (en) 1989-08-30

Family

ID=19851082

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA888996A ZA888996B (en) 1987-12-12 1988-11-30 New 11-arylsteroid compounds

Country Status (16)

Country Link
US (1) US4921845A (en)
EP (1) EP0321010B1 (en)
JP (1) JP2768707B2 (en)
KR (1) KR970009592B1 (en)
CN (1) CN1019807B (en)
AT (1) ATE85342T1 (en)
AU (1) AU613433B2 (en)
CA (1) CA1301162C (en)
DE (1) DE3878198T2 (en)
DK (1) DK168444B1 (en)
ES (1) ES2053714T3 (en)
FI (1) FI89056C (en)
IE (1) IE61848B1 (en)
NZ (1) NZ227269A (en)
PT (1) PT89185B (en)
ZA (1) ZA888996B (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE172469T1 (en) * 1989-08-04 1998-11-15 Schering Ag 11 BETA-ARYL-GONA-4,9-DIENE-3-ONE
FR2650748B1 (en) * 1989-08-08 1991-11-08 Roussel Uclaf NOVEL ESTERS OF ORGANIC ACIDS WITH ALCOHOLS DERIVED FROM 19-NOR STEROIDS AND THEIR SALTS, THEIR PREPARATION METHOD AND THE INTERMEDIATES THEREOF, THEIR APPLICATION AS MEDICAMENTS AND THE COMPOSITIONS CONTAINING THEM
DE4018168A1 (en) * 1990-06-01 1991-12-05 Schering Ag INITIAL CONNECTIONS FOR THE PRODUCTION OF 10SS-H STEROIDS AND A METHOD FOR THE PRODUCTION OF THESE OUTPUT CONNECTIONS
US5407928A (en) * 1990-08-15 1995-04-18 Schering Aktiengesellschaft 11β-aryl-gona-4,9-dien-3-ones
ZA929315B (en) * 1991-12-20 1993-05-24 Akzo Nv 17-spirofuran-3'-ylidene steroids.
CA2100514C (en) * 1992-07-29 2005-03-29 Johannes A. M. Hamersma 17-spiromethylene steroids
EP0683172B1 (en) * 1994-05-19 1997-08-13 Akzo Nobel N.V. 11,21-Bisphenyl-19-norpregnane derivatives
DE4434488A1 (en) 1994-09-14 1996-03-21 Schering Ag Steroid esters and amides, processes for their preparation and their pharmaceutical use
IL115659A (en) * 1994-10-27 2000-06-01 Akzo Nobel Nv Steroids with a 17-spiromethylene lactone or lactol group process for their preparation and pharmaceutical compositions containing them
ZA9510926B (en) 1994-12-23 1996-07-03 Schering Ag Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception
WO1997041145A1 (en) * 1996-05-01 1997-11-06 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents
US6900193B1 (en) * 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US5962444A (en) * 1998-05-29 1999-10-05 Research Triangle Institute 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6262042B1 (en) 1998-05-29 2001-07-17 Research Triangle Institute 17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
FR2789393B1 (en) * 1999-02-05 2001-10-12 Centre Nat Rech Scient STEROID LACTOL
DE60121928T2 (en) * 2000-03-31 2007-03-01 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services PROCESS FOR THE PREPARATION OF THE TRANS-4-N-BUTYLCYCLOHEXANOIC CANE AND ANDECANOIC ACID ESTERS OF (7-ALPHA, 11-BETA) -DIMETHYL-17 BETA-HYDROXY-4-ESTRENE-3-ONE AND THEIR MEDICINIC APPLICATION
CA2516319C (en) * 2003-02-28 2012-09-18 The Government Of The United States Of America, As Represented By The Se Cretary, Department Of Health And Human Services Method for preparing 17.alpha.-acetoxy-11.beta.-(4-n,n-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, intermediates thereof, and methods for the preparation of such intermediates
BRPI0717747A2 (en) 2006-10-24 2013-10-22 Repros Therapeutics Inc ENDOMETRIAL PROLIFERATION SUPPRESSION COMPOSITIONS AND METHODS
TWI539953B (en) 2008-04-28 2016-07-01 瑞波若斯治療學公司 Compositions and methods for treating breast cancer
MX2012010327A (en) 2010-03-22 2012-11-16 Repros Therapeutics Inc Compositions and methods for non-toxic delivery of antiprogestins.

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA8231B (en) * 1981-01-09 1982-11-24 Roussel Uclaf New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained
US4780461A (en) * 1983-06-15 1988-10-25 Schering Aktiengesellschaft 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same
DE3347126A1 (en) * 1983-12-22 1985-07-11 Schering AG, 1000 Berlin und 4709 Bergkamen 11SS-ARYL-ESTRADIENE, THEIR PRODUCTION AND THE PHARMACEUTICAL PREPARATIONS CONTAINING THEM
AU580843B2 (en) * 1985-02-07 1989-02-02 Schering Aktiengesellschaft 11``-phenyl-gonanes, their manufacture and pharmaceutical preparations containing them
GB8513723D0 (en) * 1985-05-31 1985-07-03 Erba Farmitalia 11-beta substituted steroids

Also Published As

Publication number Publication date
ATE85342T1 (en) 1993-02-15
AU2646988A (en) 1989-06-15
PT89185B (en) 1993-06-30
CA1301162C (en) 1992-05-19
KR890009968A (en) 1989-08-05
FI89056C (en) 1993-08-10
IE61848B1 (en) 1994-11-30
FI885717A0 (en) 1988-12-09
DK688088A (en) 1989-06-13
FI885717A (en) 1989-06-13
IE883565L (en) 1989-06-12
PT89185A (en) 1989-12-29
JPH01211597A (en) 1989-08-24
EP0321010B1 (en) 1993-02-03
NZ227269A (en) 1990-06-26
CN1019807B (en) 1992-12-30
DE3878198D1 (en) 1993-03-18
US4921845A (en) 1990-05-01
KR970009592B1 (en) 1997-06-14
DE3878198T2 (en) 1993-06-24
DK168444B1 (en) 1994-03-28
JP2768707B2 (en) 1998-06-25
AU613433B2 (en) 1991-08-01
DK688088D0 (en) 1988-12-09
ES2053714T3 (en) 1994-08-01
EP0321010A1 (en) 1989-06-21
CN1034731A (en) 1989-08-16
FI89056B (en) 1993-04-30

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